olvanil [Ligand Id: 2488] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL76903 (NE-19550, Olvanil, TCMDC-124289) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| TRPV2/Transient receptor potential cation channel subfamily V member 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2863] [GtoPdb: 508] [UniProtKB: Q9WUD2] | ||||||||
| ChEMBL | Antagonist activity at recombinant rat TRPV2 expressed in HEK293 cells assessed as inhibition of CBD-induced Ca2+ levels preincubated for 5 mins followed by agonist addition by Fuo-4-AM based spectrofluorimetry | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (2018) 61: 8255-8281 [PMID:30176215] |
| ChEMBL | Antagonist activity at recombinant rat TRPV2 expressed in HEK293 cells assessed as inhibition of LPC-induced Ca2+ levels preincubated for 5 mins followed by agonist addition by Fuo-4-AM based spectrofluorimetry | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (2018) 61: 8255-8281 [PMID:30176215] |
| TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] | ||||||||
| GtoPdb | - | - | 7.7 | pEC50 | 19.9 | nM | EC50 | Eur J Pharmacol (2001) 417: 51-8 [PMID:11301059] |
| ChEMBL | Concentration necessary to induce a relative half-maximal response measured by the entry of [Ca2+] into human embryonic kidney HEK293 cells overexpressing the human VR1 | F | 9.3 | pEC50 | 0.5 | nM | EC50 | J Med Chem (2002) 45: 3739-3745 [PMID:12166946] |
| TRPV1 in Mouse [GtoPdb: 507] [UniProtKB: Q704Y3] | ||||||||
| GtoPdb | - | - | 8.4 | pEC50 | - | - | - | Neurosci Lett (2004) 370: 55-60 [PMID:15489017] |
| TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433] | ||||||||
| ChEMBL | Displacement of [3H]RTX from rat TRPV1 expressed in CHO cells | B | 6.85 | pKi | 142 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 5227-5231 [PMID:22796184] |
| ChEMBL | Agonist activity at rat TRPV1 expressed in CHO cells assessed as calcium uptake | F | 6.69 | pEC50 | 202 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 5227-5231 [PMID:22796184] |
| GtoPdb | - | - | 8.1 | pEC50 | - | - | - | Br J Pharmacol (2000) 130: 916-22 [PMID:10864900] |
| GPR119 in Human [GtoPdb: 126] [UniProtKB: Q8TDV5] | ||||||||
| GtoPdb | - | - | 5.1 | pEC50 | - | - | - | Mol Endocrinol (2010) 24: 161-70 [PMID:19901198] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
